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정병화(Byung Hwa Jung),엄기동(Khee Dong Eom),유영숙(Young Soo Yoo),정봉철(Bong Chul Chung),박종세(Jong Sei Park) 대한약학회 1992 약학회지 Vol.36 No.1
The metabolic profile of triprolidine, 2-[1-(4-methylphenyl)-3-(1-pyrrolidinyl-1-propenyl)] pyridine, was determined in rat urine and bile. The free fractions of urinary and biliary extracts were obtained without hydrolysis, and the conjugated fractions of extracts were obtained with enzyme hydrolysis using beta-glucuronidase from Escherichia coli. The mixture of N-methyl-N-trimethylsilyltrifluoroacetamide/trimethylsilyl choloride(100 : 1, v/v) was used to derivatize the extracts and then anaylzed by gas chromatography/mass spectrometry. Hydroxymethyltriprolidine, hydroxytriprolidine, triporolidine carboxylic acid, dihydroxytriprolidine 1, dihydroxytriprolidine 2, oxotriprolidine carboxylic acid and unchanged triprolidine were detected in rat urine and bile, which were obtained after oral treatment with triprolidine hydrochloride. The maximum urinary excretion rate of triprolidine and hydroxymethyltriprolidine which were extracted from free fraction was at 1 to 2 hours after drug administration . Hydroxymethyltriprolidine was detected in conjugated fraction, and the maximum urinary excretion rate of that metabolite was at 2 to 3 hours in rat. In rat bile analysis, triprolidine was detected only in free fraction and its biliary excretion rate showed the maximum within 30 minutes after drug administration and decreased continuously thereafter. The excretion percentage of triprolidine and hydroxymethyltriprolidine to the initial dose of the parent drug in bile and urine of rats were all low.